2. Anti-infection Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. HCV HCV Protease SARS-CoV DNA/RNA Synthesis
  4. Simeprevir sodium

Simeprevir sodium  (Synonyms: 西咪匹韦钠; TMC435 sodium; TMC435350 sodium)

目录号: HY-10241A
产品使用指南 技术支持

Simeprevir (TMC435; TMC435350) sodium 是一种有效、高特异性且具有口服活性的丙型肝炎病毒 (HCV) NS3/4A蛋白酶抑制剂，Ki 值为 0.36 nM，并抑制 HCV 复制，EC50 值为 7.8 nM。Simeprevir sodium 还能有效抑制 SARS-CoV-2 的复制，并与瑞德西韦 (Remdesivir) 具有协同作用。Simeprevir sodium 可抑制 SARS-CoV-2 的主要蛋白酶 (Mpro) 和 RNA 依赖性 RNA 聚合酶 (RdRp)，并调节宿主免疫反应。

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Simeprevir sodium Chemical Structure

Simeprevir sodium Chemical Structure

CAS No. : 1241946-89-3

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Simeprevir sodium 的其他形式现货产品:

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Simeprevir sodium 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 42 篇科研文献

WB

    Simeprevir sodium purchased from MCE. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065.  [Abstract]

    Huh7.5 cells are infected with HCV and simultaneously treated with 7f (10 μM) or DAA (0.04 μM Simeprevir, 0.08 μM Sofosbuvir, or 16 pM Daclatasvir) or 7f plus DAA.

    Simeprevir sodium purchased from MCE. Usage Cited in: Biomed Res Int. 2017;2017:1236801.  [Abstract]

    Huh7.5 (HCV+) cells are treated with 1 μM of Simeprevir or solvent control. At 24 hours, the cells are washed and continuously incubated with fresh culture media containing drugs again for 48 hours. The cultural supernatants are then harvested and directly incubated to naïve Huh7.5 cells. After been passaged 1~3 times, the newly infected cells are treated with 1 μM of Simeprevir for 72 hours. Intracellular proteins are extracted and detected with WB.

    Simeprevir sodium purchased from MCE. Usage Cited in: Int J Radiat Oncol Biol Phys. 2016 Nov 15;96(4):867-876.  [Abstract]

    Simeprevir inhibits DNA damage repair following irradiation. U251, BT474, and HepG2 cells are pretreated with Simeprevir or DMSO and irradiated at a dose of 6 Gy. After 6 hours, prolongation of γH2AX foci is detected in Simeprevir-treated cells along with decreased phosphorylation of DNA-PKcs, indicating impaired nonhomologous end-joining repair.

    Simeprevir sodium purchased from MCE. Usage Cited in: J Med Chem. 2016 Nov 23;59(22):10268-10284.  [Abstract]

    Huh7.5 cells are infected with HCV (45 IU/cell) and simultaneously treated with Simeprevir (A, 0.025 μM), Sofosbuvir (B, 0.1 μM), or Daclatasvir (C, 16 pM) alone or with 1 (6.25 μM).

    Simeprevir sodium purchased from MCE. Usage Cited in: College of Medicine/School of Medicine. Seoul National University. 2016 Aug.

    Pharmacologic inhibition of PI4KIIIα using Simeprevir increases the radiosensitivity in U251 cells.

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Simeprevir (TMC435; TMC435350) sodium is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir sodium inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir sodium also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir sodium inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][4].

    IC50 & Target

    Ki: 0.36 nM (HCV NS3/4A protease)[1]
    EC50: 7.8 nM (HCV replication)[1]
    IC50: 9.6±2.3 μM (SARS-CoV-2 Mpro), 5.5±0.2 μM (SARS-CoV-2 RdRp)[4]
    体外研究
    (In Vitro)

    Simeprevir (TMC435) inhibits HCV in a dose-dependent manner in Huh7-Luc cells, with EC50 and EC90 values of 8 nM and 24 nM, respectively[2].
    Simeprevir (TMC435) inhibits NS3/4A proteases from HCV genotypes 1 to 6 with IC50s of 1/0.9/7/30/1.5/2.2/1.6 nM for 1a/1b/2b/3a/4/5/6, respectively[3].
    Simeprevir inhibits SARS-CoV-2 in Vero E6 cells with an IC50 of 9.6±2.3 μM and 5.5±0.2 μM for Mpro and RdRp, respectively[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Simeprevir sodium 相关抗体:
    体内研究
    (In Vivo)

    Simeprevir (TMC435) has moderate terminal elimination half-life (t1/2=1.5 h and 4.1 h for rat (3 mg/kg, p.o.), monkey (3 mg/kg, p.o.))[3].
    Simeprevir (TMC435350) exhibits a medium-slow rate of absorption, well distribution with the high concentration observed in the liver, and a low clearance[1].
    Pharmacokinetic Parameters of Simeprevir (TMC435350) in male Sprague-Dawley rats[1].

    IV (2 mg/kg) PO (10 mg/kg)
    CL (L/h/kg) 0.505
    Vdss (h) 0.49
    AUC0-24 (μM·h) 5.21 2.79
    Cmax (μM) 0.73
    Tmax (h) 3.0
    T1/2 (h) 2.8
    F (%) 11
    Liver/plasma ratio at 6 h 63.5 32

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Sprague-Dawley (SD) rats and cynomolgus monkeys[3]
    Dosage: 3 mg/kg
    Administration: PO; single dosage
    Result: Time at which peak concentration (Tmax) of 1 hour and 2 hour for rat and monkey, respectively.
    Concentration at 24 h after dosing (C24 h) of 0.9 and 2.3 ng/mL for rat and monkey, respectively.
    AUC0-24h=1173 and 1409 ng·h/mL for rat and monkey, respectively.
    Clinical Trial
    Formula

    C38H47N5NaO7S2
    CAS 号
    中文名称

    西咪匹韦钠
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Simeprevir sodium 相关分类

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Simeprevir1241946-89-3TMC435TMC435350西咪匹韦钠TMC 435TMC-435TMC 435350TMC-435350HCVHCV ProteaseSARS-CoVDNA/RNA SynthesisHepatitis C virusSARS coronavirusVirus replicationRemdesivirRNA-dependent RNA polymeraseRdRpimmune responsesHuh7-LucInhibitorinhibitorinhibit

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